Synthesis and Biological Evaluation of Strictosamide Derivatives with Improved Antiviral and Antiproliferative Activities

Chem Biol Drug Des. 2015 Oct;86(4):523-30. doi: 10.1111/cbdd.12515. Epub 2015 Feb 12.

Abstract

A series of novel derivatives of strictosamide were synthesized and biologically evaluated. Most of the new compounds exhibited improved activities than the parent compound strictosamide. Among them, compounds Ib and If possessed antiviral activities against influenza A virus (A/Jinan/15/90) with IC50 values of 4.12 and 12.35 μg/mL, respectively. Compound Ie possessed antiviral activity against respiratory syncytial virus (RSV) with an IC50 value of 9.58 μg/mL. Both compounds IIc and IId had moderate antiproliferative effects against five human cancer cell lines. The preliminary structure-activity relationships were also concluded. This study provides a promising new template with potential antiviral activity.

Keywords: SARs; antiproliferative effect; antiviral activity; derivatives; strictosamide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents* / chemical synthesis
  • Antiviral Agents* / chemistry
  • Antiviral Agents* / pharmacology
  • Cell Proliferation / drug effects*
  • Dogs
  • Hep G2 Cells
  • Humans
  • Influenza A virus*
  • Influenza, Human / drug therapy*
  • Influenza, Human / metabolism
  • Madin Darby Canine Kidney Cells
  • Respiratory Syncytial Virus Infections / drug therapy*
  • Respiratory Syncytial Virus Infections / metabolism
  • Respiratory Syncytial Viruses*
  • Vinca Alkaloids* / chemical synthesis
  • Vinca Alkaloids* / chemistry
  • Vinca Alkaloids* / pharmacology

Substances

  • Antiviral Agents
  • Vinca Alkaloids
  • strictosamide